厄洛替尼

厄洛替尼（英語：Erlotinib，商品名：Tarceva，特罗凯）是用于治疗非小细胞肺癌（NSCLC）、胰腺癌等几种癌症的药物，作为一种酪氨酸激酶抑制剂作用于表皮生长因子受体，由罗氏公司生产。

厄洛替尼

臨床資料
商品名	Tarceva
AHFS/Drugs.com	Monograph
MedlinePlus	a605008
核准狀況	歐 EMA: yes 美 FDA: Erlotinib
给药途径	Oral tablets
ATC碼	L01XE03 (WHO)
法律規範狀態
法律規範	英：处方药（℞-only） (POM) 美：处方药（℞-only）
藥物動力學數據
生物利用度	59%
血漿蛋白結合率	95%
药物代谢	Hepatic (mainly CYP3A4, less CYP1A2)
生物半衰期	36.2 hrs (median)
排泄途徑	>98% as metabolites, of which >90% via faeces, 9% via urine
识别信息
IUPAC命名法 N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy) quinazolin-4-amine
CAS号	183321-74-6  Y
PubChem CID	176870
DrugBank	DB00530 Y
ChemSpider	154044 Y
UNII	J4T82NDH7E
KEGG	D07907 Y
ChEBI	CHEBI:114785 Y
ChEMBL	ChEMBL553 Y
CompTox Dashboard (EPA)	DTXSID8046454
ECHA InfoCard	100.216.020
化学信息
化学式	C22H23N3O4
摩尔质量	393.436 g/mol
3D模型（JSmol）	交互式图像
SMILES COCCOc1cc2c(cc1OCCOC)ncnc2Nc3cccc(c3)C#C
InChI InChI=1S/C22H23N3O4/c1-4-16-6-5-7-17(12-16)25-22-18-13-20(28-10-8-26-2)21(29-11-9-27-3)14-19(18)23-15-24-22/h1,5-7,12-15H,8-11H2,2-3H3,(H,23,24,25) Y Key:AAKJLRGGTJKAMG-UHFFFAOYSA-N Y

藥物合成

• 第一種合成路徑

• 第二種合成路徑

外部链接

• Official Tarceva website （页面存档备份，存于互联网档案馆）
• Tarceva Discussion Group for Cancer Patients （页面存档备份，存于互联网档案馆）
• Sordella R, Bell DW, Haber DA, Settleman J. Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science. August 2004, 305 (5687): 1163–7. PMID 15284455. doi:10.1126/science.1101637. .
• Genzyme "Genzyme Launches Exclusive Lung Cancer Test" Press Release September 27, 2005
• "Determinants of Tumor Response and Survival With Erlotinib in Patients With Non-Small-Cell Lung Cancer （页面存档备份，存于互联网档案馆）, Journal of Clinical Oncology, August 15, 2004.
• October 2003 issue of Lung Cancer Frontiers on rash/effectiveness correlation
• FAQ: I started an EGFR inhibitor two weeks ago but haven’t developed a rash. Does this mean it’s not working?, Dr. Howard L. (Jack) West, M.D., GRACE（页面存档备份，存于互联网档案馆）, February 21, 2011 (directed toward the layperson).
• http://www.cancer.gov/clinicaltrials/results/lung-and-erlotinib0604l
• https://web.archive.org/web/20081012081613/http://www.roche.com/med-cor-2007-10-22
• https://web.archive.org/web/20110726060413/http://www.roche.com/med-cor-2009-05-30b
• https://web.archive.org/web/20120918193637/http://www.cipla.com/whatsnew/news.htm#27apr09
• https://web.archive.org/web/20120918193637/http://www.cipla.com/whatsnew/news.htm#20mar08